Description
A 5-HT3 receptor antagonist (Ki = 3.9 nM) with antiemetic activity; selective for 5-HT3 over 5-HT4 receptors (Ki = >1,000 nM); increases the latency to first vomiting episodes and reduces the number of vomiting episodes in a canine model of cisplatin-induced emesis at 0.3, 1, and 3 mg/kg, p.o.; increases the latency to first vomiting episode and reduces the number of vomiting and retching episodes in a ferret model of emesis induced by doxorubicin and cyclophosphamide at 0.1, 0.3, and 1 mg/kg